Department of Pharmacy and Health and Nutrition Sciences, University of Calabria, 87036 Arcavacata di Rende (CS), Italy.
Molecules. 2020 Aug 2;25(15):3535. doi: 10.3390/molecules25153535.
Psoriasis is one of the most common human skin disorders. Although its pathogenesis is complex and not completely know, the hyperactivation of the immune system seem to have a key role. In this regard, among the most effective systemic therapeutics used in psoriasis, we find cyclosporine, an immunosuppressive medication. However, one of the major problems associated with the use of cyclosporine is the occurrence of systemic side effects such as nephrotoxicity, hypertension, etc. The present work fits in this context and its aim is the design of suitable platforms for cyclosporine topical release in psoriasis treatment. The main objective is to achieve local administration of cyclosporine in order to reduce its systemic absorption and, consequently, its side effects. In order to improve dermal penetration, solid lipid nanoparticles (SLNs) are used as carriers, due to their lipophilicity and occlusive properties, and naringenin and linolenic acid are chosen, due to their properties, as starting materials for SLNs design. In order to have dermatological formulations and further modulate drug release, SLNs are incorporated in several topical vehicles obtaining gels with different degree of lipophilicity. Potential applications for psoriasis treatment were evaluated by considering the encapsulation efficiency, release profiles, in vitro skin permeation, and anti-inflammatory effects.
银屑病是最常见的人类皮肤疾病之一。虽然其发病机制复杂且不完全清楚,但免疫系统的过度激活似乎起着关键作用。在这方面,在银屑病最有效的系统性治疗药物中,我们发现了环孢素,一种免疫抑制剂。然而,使用环孢素的主要问题之一是会出现全身副作用,如肾毒性、高血压等。本工作正是在此背景下进行的,其目的是设计合适的平台,用于银屑病治疗中环孢素的局部释放。主要目标是实现局部给予环孢素,以减少其全身吸收,从而降低其副作用。为了提高透皮能力,使用固体脂质纳米粒 (SLN) 作为载体,因为其具有亲脂性和封闭性,并且选择柚皮素和亚油酸作为 SLN 设计的起始材料,因为它们具有这些特性。为了获得具有不同亲脂性的局部用制剂并进一步调节药物释放,将 SLN 掺入几种局部用载体中,得到具有不同亲脂性的凝胶。通过考虑包封效率、释放曲线、体外皮肤渗透和抗炎作用,评估了潜在的银屑病治疗应用。